LORMETAZEPAM

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Created Sep 2019 | Updated Nov 2020

LORMETAZEPAM

  • [NOCTAMID]

Noctamid | Ergocalm | Loramet | Dilamet | Dormagen | Sedaben | Stilaze | Nocton | Pronoctan | Noctamide | Loretam | Minias | Aldosomnil | Noctofer

DEA CODE 2774: Schedule 4

Lormetazepam (or methyl-lorazepam), possesses hypnotic, anxiolytic, sedative and skeletal muscle relaxant properties. Lormetazepam is not approved for sale in the United States or Canada, though it is licensed in the Netherlands as 1 and 2 mg tablets, under the brand names Loramet and Noctamid and as generic, available from several different manufacturers. Lormetazepam is a short-acting benzodiazepine and is sometimes used in patients who have difficulty in maintaining sleep or falling asleep. Lormetazepam binds to the benzodiazepine receptor which in turn enhances the effect of the GABAA receptor producing its therapeutic effects as well as adverse effects. Lormetazepam appears to be more selective in the type of benzodiazepine receptor it binds to showing a higher affinity for the omega 1 receptor which is responsible for sedation. Changes in electroencephalography can therefore be used to measure the sedative sleep promoting properties of lormetazepam.

Lormetazepam
Duration:

Relatively rare prescription benzodiazepine. Short acting with a short half life. Generally only seen in the Netherlands. Sedative, hypnotic and anxiolytic.

RouteOnsetDurationAfter Effects
Tripsit Factsheets
All ROAs:10-30 minutes4-8 hours1-24 hours
Lormetazepam Duration
Avoid:
All other CNS depressants.

Lormetazepam will help you to sleep. You will be prescribed a short course of treatment only. The effects of lormetazepam can last into the following day; it can affect your reactions and your ability to drive. Do not drive and do not use tools or machines while affected.

Poor sleep (insomnia) is fairly common but does not usually last for long. If you have problems sleeping, it may mean that you have difficulty getting off to sleep, or you may wake up for long periods during the night, or you may wake up too early in the morning. 'Sleeping tablets' are considered a last resort, but are sometimes prescribed for a short period of time to help with a particularly bad spell of insomnia. Lormetazepam works by affecting the way certain brain chemicals (neurotransmitters) transmit messages. This has a calming effect and helps you to sleep. It works well in the short term, but lormetazepam is not normally advised for more than 1-3 weeks. If you take it for longer, the medicine may lose its effect (you may become tolerant to the effect), and if you stop it you may develop withdrawal symptoms. You may need to keep taking the medicine to avoid the withdrawal symptoms.

Lormetazepam is used for the short-term treatment of severe insomnia. It decreases the time taken to fall asleep and number of times you wake in the night, as well as increasing the total amount of time spent sleeping. However, it is only suitable for short-term treatment of insomnia as it has a high potential for dependence and addiction. As lormetazepam remains active in the body for many hours, drowsiness may also last into the next day. Lormetazepam works by acting on receptors in the brain called GABA receptors. This causes the release of a neurotransmitter called GABA in the brain. GABA is a neurotransmitter that acts as a natural 'nerve-calming' agent. It helps keep the nerve activity in the brain in balance, and is involved in inducing sleepiness, reducing anxiety and relaxing muscles. As lormetazepam increases the activity of GABA in the brain, it increases its calming effect and results in sleepiness, a decrease in anxiety and relaxation of muscles.

Lormetazepam binds to the benzodiazepine receptor which in turn enhances the effect of the GABAA receptor producing its therapeutic effects as well as adverse effects. When lormetazepam binds to the benzodiazepine receptor sites in sufficient quantities it produces sedation which is used clinically as a therapeutic treatment for insomnia. Lormetazepam alters the brain electrical activity which has been studied via EEG readings. Lormetazepam appears to be more selective in the type of benzodiazepine receptor it binds to showing a higher affinity for the omega 1 receptor which is responsible for sedation. Changes in EEG can therefore be used to measure the sedative sleep promoting properties of lormetazepam.

Lormetazepam, or methyl-lorazepam, is a drug which is a short to intermediate acting 3-hydroxy benzodiazepine derivative. It possesses hypnotic, anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. Lormetazepam is considered a hypnotic benzodiazepine and is officially indicated for moderate to severe insomnia. Lormetazepam is a short-acting benzodiazepine and is sometimes used in patients who have difficulty in maintaining sleep or falling asleep. Hypnotics should only be used on a short-term basis or, in those with chronic insomnia, on an occasional basis.


Lormetazepam may cause mild to severe side effects. If you feel that your episodes of drowsiness, lightheadedness, confusion, vertigo, visual disturbance, and incontinence are more than you can handle, talk to your doctor about possible dosage adjustment or the use of a different drug altogether. Also, take note of severe and serious side effects including seizures, hallucinations, and painful tremors. Any sign that your symptoms of side effects are overpowering the benefits that you get from the drug must be brought to the attention of a qualified professional.

Patients who use Lormetazepam must also note that the drug is only advisable for short-term use. After a period of time, Lormetazepam may no longer have any effect to your body as it becomes used to it. If you are under Lormetazepam medication for a long time, talk to your doctor before stopping the drug. Stopping abruptly may cause withdrawal symptoms.

Elderly:
Sleep architecture changes with age, both in terms of efficiency and total duration of sleep. Hypnotic benzodiazepines promote rapid onset of sleep, uninterrupted sleep and longer duration of sleep in the absence of carryover sedation the following morning; therefore, these may be appropriate for use in older patients. This study was performed to evaluate the efficacy and safety of lormetazepam in elderly patients with primary insomnia when used in association with sleep hygiene training (SHT). Management of insomnia in the elderly appears to have a better outcome when pharmacotherapy is combined with SHT rather than SHT alone. The earlier improvement in sleep quality with lormetazepam when used in combination with a sleep training programme may help to maintain adherence to treatment.

Breastfeeding:
Lormetazepam has low levels in breastmilk and a short half-life relative to many other benzodiazepines. Limited evidence from nursing mothers indicates that lorazepam does not cause any adverse effects in breastfed infants with usual maternal dosages. No special precautions are required.

Breastfeeding:

Summary of Use During Lactation:
Lormetazepam is not approved for marketing in the United States by the U.S. Food and Drug Administration.

Lormetazepam has low levels in breastmilk and a short half-life relative to many other benzodiazepines.

Limited evidence from nursing mothers indicates that lorazepam does not cause any adverse effects in breastfed infants with usual maternal dosages.

No special precautions are required.

Alternate Drugs to Consider:

Overdose:
Lormetazepam is practically insoluble (in water) and a very weakly acidic compound (based on its pKa). Lormetazepam can be found in potato, which makes lormetazepam a potential biomarker for the consumption of this food product. Lormetazepam is a non-carcinogenic (not listed by IARC) potentially toxic compound. Lormetazepam is a drug which is used for the treatment of short-term insomnia. The primary manifestation of overdosage ranges from drowsiness to coma and symptoms may include ataxia, hypotension, hypotonia, respiratory depression which may lead to death.

General warnings for Lormetazepam:

Contraindications:
Acute pulmonary insufficiency, respiratory depression, sleep apnoea, phobic or obsessional states, chronic psychosis, myasthenia gravis. Severe hepatic impairment. Lactation.

Warnings:
Chronic pulmonary insufficiency. Renal impairment. Mild to moderate hepatic impairment. History of drug or alcohol abuse. Personality disorders. Elderly. Withdraw gradually. Pregnancy.

Interactions:
Alcohol, CNS depressants, anticonvulsants, CYP3A4 inhibitors or inducers (e.g. cimetidine, rifampicin).

Adverse Effects:
Drowsiness, which may continue into the following day. Muscle weakness, ataxia, confusion, vertigo, GI upset, visual disturbances, rash, impaired alertness and dexterity, headache, urinary retention, changes in libido. Anterograde amnesia. Rarely blood disorders, jaundice. Dependence.

EMC PDF Lormetazepam

Medsafe PDF Lormetazepam

It was patented in 1961 and came into medical use in 1980. Lormetazepam is not approved for sale in the United States or Canada. It is licensed in the UK as 0.5 and 1 mg tablets for short-term treatment (2-4 weeks) of moderately severe insomnia. Hypnotics should only be used on a short-term basis or, in those with chronic insomnia, on an occasional basis. In a sleep study, 1 mg lormetazepam increased total sleep time, reduced wakefulness, but did not alter REM sleep. However, at 2 mg doses, there were significant increases in stage 3 sleep and reductions in REM sleep. Rebound effects have been reported after chronic use including rebound REM. Although lormetazepam has been associated with adversely affecting immediate and delayed recall memory functions, studies have shown that lormetazepam's amnesic properties may be lesser compared to other hypnotic benzodiazepines. Benzodiazepines require special precaution if used during pregnancy, in children, in alcohol- or drug-dependent individuals and individuals with comorbid psychiatric disorders. Lormetazepam may be unsuitable for the elderly due to residual effects on memory and body sway which may result in falls. Lormetazepam causes impaired driving skills, thus caution is required in individuals who drive or operate machinery. The risks of tolerance, dependence, and withdrawal are very low when the drug is used for 2-4 weeks only, and lormetazepam is generally a safe and effective drug when used for no longer than 2-4 weeks.

  
Role of Lormetazepam in the Treatment of Insomnia in the Elderly - The remaining 30 patients (14 male, 16 female) had a mean age of 72 years and were randomised to receive lormetazepam + SHT or SHT only. The two groups were well balanced with respect to baseline ...
Sunday January 28, 2024 - medscape.com

Insomnia in General Practice - It is useful to outline the principal characteristics of these agents and to examine in-depth the three drugs most frequently prescribed: two classic benzodiazepines, triazolam and lormetazepam ...
Friday January 19, 2024 - medscape.com

Computerized Physician Order System (CPOE) - were for drugs that are categorized in the list as potentially inadequate for older patients. These prescriptions included in particular preparations containing lormetazepam >0.5 mg/d (1861 ...
Friday March 25, 2016 - aerzteblatt.de

Acebrophylline Interaction with other Drugs - Acebrophylline is prescribed to reduce the irritation, swelling, and narrowing of the bronchial tubes in patients with asthma, severe or chronic bronchitis, chronic obstructive pulmonary disease ...
Tuesday April 21, 2020 - medindia.net

Flunarizine Interaction with other Drugs - Flunarizine is a calcium channel blocker, prescribed for migraine occlusive peripheral vascular disease, vertigo of central and peripheral origin and as an adjuvant in the therapy of epilepsy.
Thursday October 21, 2021 - medindia.net

  
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